有前途的抗细菌剂:水杨基肼

IF 3.6 3区 医学 Q2 CHEMISTRY, MEDICINAL
Oya Unsal Tan, Sıva Krıshna Vagolu, Tone Tønjum, Ozan Kaplan, Rahime Simsek
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引用次数: 0

摘要

结核病仍然是一项重大的全球卫生挑战,强调迫切需要新的治疗方案。本研究合成了一系列水杨基肼衍生物,并用光谱技术对其进行了表征。测定其对结核分枝杆菌H37Rv的抑菌活性。在所合成的35个化合物中,有9个化合物表现出显著的抑制活性,其MIC值在0.78 ~ 50 μM之间。这些活性分子对临床异烟肼耐药(携带inhA启动子和/或katG突变)和多药耐药(MDR)结核分枝杆菌菌株进行了进一步评估。由2-溴-4-硝基水杨醛衍生的化合物对H37Rv的MIC值为0.78 μM,对inhA +、katG +和MDR的MIC值分别为6.25、1.56和1.56 μM。分子对接研究也用于研究活性化合物与靶酶InhA的相互作用。总之,研究结果表明,水杨柳肼衍生物为开发对药敏和耐药结核分枝杆菌均有效的新型抗结核药物提供了有前途的先导结构。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Promising Antimycobacterial Agents: Salicylidenehydrazines

Tuberculosis (TB) remains a major global health challenge, underscoring the urgent need for new therapeutic options. In this study, a series of salicylidenehydrazine derivatives were synthesized and characterized using spectroscopic techniques. Their antimycobacterial activity was assessed against Mycobacterium tuberculosis H37Rv. Among the 35 synthesized compounds, nine demonstrated significant inhibitory activity, with MIC values ranging from 0.78 to 50 μM. These active molecules were further evaluated against clinical isoniazid-resistant (bearing inhA promoter and/or katG mutations) and multidrug-resistant (MDR) M. tuberculosis strains. A particularly potent compound derived from 2-bromo-4-nitrosalicylaldehyde exhibited an MIC of 0.78 μM against H37Rv and demonstrated low MIC values of 6.25, 1.56, and 1.56 μM against the inhA + , katG + , and MDR strains, respectively. Molecular docking studies were also conducted to investigate the interaction of active compounds with the target enzyme InhA. Overall, the results indicate that salicylidenehydrazine derivatives represent promising lead structures for the development of new anti-TB agents effective against both drug-sensitive and drug-resistant M. tuberculosis strains.

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来源期刊
Archiv der Pharmazie
Archiv der Pharmazie 医学-化学综合
CiteScore
7.90
自引率
5.90%
发文量
176
审稿时长
3.0 months
期刊介绍: Archiv der Pharmazie - Chemistry in Life Sciences is an international journal devoted to research and development in all fields of pharmaceutical and medicinal chemistry. Emphasis is put on papers combining synthetic organic chemistry, structural biology, molecular modelling, bioorganic chemistry, natural products chemistry, biochemistry or analytical methods with pharmaceutical or medicinal aspects such as biological activity. The focus of this journal is put on original research papers, but other scientifically valuable contributions (e.g. reviews, minireviews, highlights, symposia contributions, discussions, and essays) are also welcome.
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